Cytotoxic activity of azelaic acid against human melanoma primary cultures and established cell lines.
The in vitro cytotoxic activity of azelaic acid was studied with 25 human melanoma primary cultures and with 5 established cell lines characterized by different contents of melanotic pigment. A dose-dependent antiproliferative effect was observed in both the experimental systems, even though cell lines displayed a slightly greater susceptibility to the compound, with ID50 values generally lower than those for fresh human tumors. Our results do not demonstrate a clear difference between melanotic and non-melanotic melanomas in sensitivity to azelaic acid. The early interference of azelaic acid on nucleic acid metabolism was investigated additionally with 15 human melanoma primary cultures. There were significant inhibitions of RNA and DNA synthesis in a remarkable percentage of tumors, at the highest concentrations of the compound. Moreover, cell proliferation of tumors that showed these antimetabolic effects was always significantly depressed by lower drug concentration as well as by the highest.
Zaffaroni
N
N
Istituto Nazionale per lo Studio e la Cura dei Tumori, Milano, Italy.
Villa
R
R
Silvestro
L
L
Sanfilippo
O
O
Silvestrini
R
R
D000970:Antineoplastic Agents / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects*; D004261:DNA Replication / Q000187:drug effects; D003998:Dicarboxylic Acids / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008207:Lymphatic Metastasis; D008545:Melanoma / Q000473:pathology*; D012334:RNA, Neoplasm / Q000096:biosynthesis / Q000187:drug effects; D012878:Skin Neoplasms / Q000473:pathology / Q000556:secondary; D014407:Tumor Cells, Cultured / Q000166:cytology* / Q000187:drug effects
D000970:Antineoplastic Agents; D003998:Dicarboxylic Acids; D012334:RNA, Neoplasm; C010038:azelaic acid